Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变,导致细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 358 | 现货 | ||
2 mg | ¥ 519 | 现货 | ||
5 mg | ¥ 863 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,630 | 现货 | ||
50 mg | ¥ 3,860 | 现货 | ||
100 mg | ¥ 5,490 | 现货 | ||
500 mg | ¥ 10,900 | 现货 |
产品描述 | Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. |
靶点活性 | Chk1:<1 nM, Chk2:8 nM |
体外活性 | LY2606368 potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells(EC50=9 nM). LY2606368 is a potent and selective ATP competitive inhibitor of Chk1(IC50 <1 nM), and also inhibits CHK2(IC50=8 nM). |
体内活性 | In xenograft tumor models, LY2606368 (15 mg/kg, s.c.) significantly inhibits tumor growth with less animal weight loss. |
细胞实验 | LY2606368 is broadly antiproliferative with IC50s of 3 nM, 3 nM, 10 nM, 37 nM, and 68 nM against U-2 OS, Calu-6, HT-29, HeLa, and NCI-H460 cell lines, respectively. LY2606368 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells. |
动物实验 | LY2606368 is formulated in vehicle consisting of 20% Captisol.Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or LY2606368 is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos. |
别名 | 5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈, LY2606368 |
分子量 | 365.39 |
分子式 | C18H19N7O2 |
CAS No. | 1234015-52-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: < 1 mg/mL (insoluble or slightly soluble)
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Prexasertib 1234015-52-1 Apoptosis Cell Cycle/Checkpoint Chk SIK Checkpoint Kinase (Chk) HT-29 S296 DNA double-stranded inhibit autophosphorylation LY-2606368 H2AX ATP-competitive HeLa MELK RSK1 CDK2 Inhibitor S516 ARK5 5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈 replication BRSK2 LY2606368 CDC25A LY 2606368 inhibitor